42082-29-1Relevant articles and documents
Synthesis and anticancer activity evaluation of naphthalene-substituted triazole spirodienones
Luo, Lan,Jia, Jing Jing,Zhong, Qiu,Zhong, Xue,Zheng, Shilong,Wang, Guangdi,He, Ling
, (2020/12/02)
Building on our previous work that discovered 1,2,4-triazole–spirodienone as a promising pharmacophore for anticancer activity, we have further diversified 1,2,4–triazole- spirodienone derivatives and synthesized a series of novel naphthalene-substituted
Design and synthesis of α-phenoxy-N-sulfonylphenyl acetamides as Trypanosoma brucei Leucyl-tRNA synthetase inhibitors
Xin, Weixiang,Li, Zezhong,Wang, Qing,Du, Jin,Zhu, Mingyan,Zhou, Huchen
, (2019/11/26)
Human African trypanosomiasis (HAT), caused by the parasitic protozoa Trypanosoma brucei, is one of the fatal diseases in tropical areas and current medicines are insufficient. Thus, development of new drugs for HAT is urgently needed. Leucyl-tRNA synthetase (LeuRS), a recently clinically validated antimicrobial target, is an attractive target for development of antitrypanosomal drugs. In this work, we report a series of α-phenoxy-N-sulfonylphenyl acetamides as T. brucei LeuRS inhibitors. The most potent compound 28g showed an IC50 of 0.70 μM which was 250-fold more potent than the starting hit compound 1. The structure-activity relationship was also discussed. These acetamides provided a new scaffold and lead compounds for the further development of clinically useful antitrypanosomal agents.
Discovery and development of a novel class of phenoxyacetyl amides as highly potent TRPM8 agonists for use as cooling agents
Noncovich, Alain,Priest, Chad,Ung, Jane,Patron, Andrew P.,Servant, Guy,Brust, Paul,Servant, Nicole,Faber, Nathan,Liu, Hanghui,Gonsalves, Nicole S.,Ditschun, Tanya L.
, p. 3931 - 3938 (2017/07/27)
The paper presents the activity trends for a novel series of phenoxyacetyl amides as human TRPM8 receptor agonists. This series encompasses in vitro activity values ranging from the micromolar to the picomolar levels. Sensory evaluation of these molecules highlights their relevance as cooling agents for oral applications. The positive outcome of the complete evaluation of N-(1H-pyrazol-3-yl)-N-(thiophen-2-ylmethyl)-2-(p-tolyloxy)acetamide resulted in its approval for Generally Recognized As Safe (GRAS) status by the Flavor & Extract Manufacturer Association (FEMA) as FEMA 4809.